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公开(公告)号：US20060040999A1
公开(公告)日：2006-02-23
申请号：US11173295
申请日：2005-07-01
申请人： Amjad Ali , Joann Napolitano , Qiaolin Deng , Zhijian Lu , Peter Sinclair , Gayle Taylor , Christopher Thompson , Nazia Quraishi , Cameron Smith , Julianne Hunt , Adrian Dowst , Yi-Heng Chen , Hong Li
发明人： Amjad Ali , Joann Napolitano , Qiaolin Deng , Zhijian Lu , Peter Sinclair , Gayle Taylor , Christopher Thompson , Nazia Quraishi , Cameron Smith , Julianne Hunt , Adrian Dowst , Yi-Heng Chen , Hong Li
IPC分类号： A61K31/421 , C07D263/16
CPC分类号： C07F7/10 , A61K31/4015 , A61K31/4166 , A61K31/4168 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K45/06 , C07D207/26 , C07D207/27 , C07D233/32 , C07D233/38 , C07D233/50 , C07D233/52 , C07D263/04 , C07D263/20 , C07D263/22 , C07D263/24 , C07D263/26 , C07D285/06 , C07D285/10 , C07D401/04 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/04 , C07D417/10
摘要： Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.
摘要翻译： 具有式I结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于升高HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。在式I化合物中，B或 R 2是具有邻芳基，杂环，苯并杂环或苯并环烷基取代基的苯基，并且在5元环上的另一个位置具有直接连接的芳族，杂环，环烷基，苯并杂环或苯并环烷基取代基 通过-CH 2 - 2连接到环上或连接到环上。
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公开(公告)号：US20210395255A1
公开(公告)日：2021-12-23
申请号：US17292511
申请日：2019-11-15
申请人： Zachary G. BRILL , Amjad ALI , Jared CUMMING , Duane DEMONG , Qiaolin DENG , Thomas H. GRAHAM , Rongze KUANG , Yeon-Hee LIM , Christopher W. PLUMMER , Jenny Lorena RICO DUQUE , Huijun WANG , Yonglian ZHANG , Kake ZHAO , Merck Sharp & Dohme Corp.
发明人： Zachary G. Brill , Amjad Ali , Jared Cumming , Duane DeMong , Qiaolin Deng , Thomas H. Graham , Rongze Kuang , Yeon-Hee Lim , Christopher W. Plummer , Jenny Lorena Rico Duque , Huijun Wang , Yonglian Zhang , Kake Zhao
IPC分类号： C07D487/04 , C07K16/28
摘要： In its many embodiments, the present invention provides certain substituted amino triazolopyrimidine and amino triazolopyrazine compounds of Formula (IA) and Formula (IB): or and pharmaceutically acceptable salts thereof, wherein, R1, R2, and R3 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and their use in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.
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公开(公告)号：US20100249024A1
公开(公告)日：2010-09-30
申请号：US12815146
申请日：2010-06-14
申请人： Amjad Ali , Joann Bohn , Qiaolin Deng , Zhijian Lu , Peter J. Sinclair , Gayle E. Taylor , Christopher F. Thompson , Nazia Quraishi
发明人： Amjad Ali , Joann Bohn , Qiaolin Deng , Zhijian Lu , Peter J. Sinclair , Gayle E. Taylor , Christopher F. Thompson , Nazia Quraishi
IPC分类号： A61K31/44 , C07C211/29 , C07C271/20 , C07D213/54 , C07D215/12 , C07D217/02 , A61K31/472 , A61K31/47 , A61K31/4412 , A61K31/404 , A61K31/343 , A61K31/381 , A61K31/42 , A61P9/10 , A61K38/28 , A61K31/455 , A61K38/26
CPC分类号： A61K31/343 , A61K31/381 , A61K31/404 , A61K31/42 , A61K31/44 , A61K31/4412 , A61K31/455 , A61K31/47 , A61K31/472 , A61K38/00 , A61K45/06 , C07C233/16 , C07C271/16 , C07C271/20 , C07C271/22 , C07C275/32 , C07C311/04 , C07C311/08 , C07C317/32 , C07D209/08 , C07D213/54 , C07D215/12 , C07D217/02 , C07D261/08 , C07D271/10 , C07D307/14 , C07D307/79 , C07D333/20 , C07D333/22 , C07D333/28 , A61K2300/00
摘要： Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula 1, A1 and A2 are each an aromatic ring, a 5-6-membered heterocyclic ring, an aromatic ring fused to a heterocyclic ring, a phenyl ring fused to a heterocyclic ring, or a cycloalkyl ring.
摘要翻译： 式I化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于培养HDL-胆固醇，降低LDL-胆固醇，以及治疗或预防动脉粥样硬化。 在式1化合物中，A1和A2各自为芳环，5-6元杂环，稠合于杂环的芳环，稠合于杂环的苯环或环烷基环。
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公开(公告)号：US07737295B2
公开(公告)日：2010-06-15
申请号：US11578694
申请日：2005-04-08
申请人： Amjad Ali , Joann Bohn , Qiaolin Deng , Zhijian Lu , Peter J. Sinclair , Gayle E. Taylor , Christopher F. Thompson , Nazia Quraishi
发明人： Amjad Ali , Joann Bohn , Qiaolin Deng , Zhijian Lu , Peter J. Sinclair , Gayle E. Taylor , Christopher F. Thompson , Nazia Quraishi
IPC分类号： C07C261/00 , C07C211/00 , A01N47/10
CPC分类号： C07C271/20 , C07C233/18 , C07C271/16 , C07C271/22 , C07C279/08 , C07C311/04 , C07C311/08 , C07C317/32 , C07D209/08 , C07D213/40 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/89 , C07D215/12 , C07D215/26 , C07D217/02 , C07D217/14 , C07D261/08 , C07D271/06 , C07D307/52 , C07D307/79 , C07D333/20 , C07D333/22 , C07D333/28
摘要： Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula 1, A1 and A2 are each an aromatic ring, a 5-6-membered heterocyclic ring, an aromatic ring fused to a heterocyclic ring, a phenyl ring fused to a heterocyclic ring, or a cycloalkyl ring.
摘要翻译： 式I化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于培养HDL-胆固醇，降低LDL-胆固醇，以及治疗或预防动脉粥样硬化。 在式1化合物中，A1和A2各自为芳环，5-6元杂环，稠合于杂环的芳环，稠合于杂环的苯环或环烷基环。
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公开(公告)号：US20100099716A1
公开(公告)日：2010-04-22
申请号：US12625783
申请日：2009-11-25
申请人： Amjad ALI , Joann M. Napolitano , Qiaolin Deng , Zhijian Lu , Peter J. Sinclair , Gayle E. Taylor , Christopher F. Thompson , Nazia Quraishi , Cameron J. Smith , Julianne A. Hunt , Adrian A. Dowst , Yi-Heng Chen , Hong Li
发明人： Amjad ALI , Joann M. Napolitano , Qiaolin Deng , Zhijian Lu , Peter J. Sinclair , Gayle E. Taylor , Christopher F. Thompson , Nazia Quraishi , Cameron J. Smith , Julianne A. Hunt , Adrian A. Dowst , Yi-Heng Chen , Hong Li
IPC分类号： A61K31/421 , C07D263/04 , C07D413/04 , A61K31/4439 , A61P9/10
CPC分类号： C07F7/10 , A61K31/4015 , A61K31/4166 , A61K31/4168 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K45/06 , C07D207/26 , C07D207/27 , C07D233/32 , C07D233/38 , C07D233/50 , C07D233/52 , C07D263/04 , C07D263/20 , C07D263/22 , C07D263/24 , C07D263/26 , C07D285/06 , C07D285/10 , C07D401/04 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/04 , C07D417/10
摘要： Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.
摘要翻译： 具有式I结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于升高HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。在式I化合物中，B或 R2是具有邻芳基，杂环，苯并杂环或苯并环烷基取代基的苯基，并且在5元环上的另一个位置具有直接连接到环上或连接到环上的芳族，杂环，环烷基，苯并杂环或苯并环烷基取代基 通过-CH2-。
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公开(公告)号：US20230054411A1
公开(公告)日：2023-02-23
申请号：US17294836
申请日：2019-11-26
申请人： Yonglian ZHANG , Amjad ALI , Jared CUMMING , Duane DEMONG , Qiaolin DENG , Thomas H. GRAHAM , Elisabeth HENNESSY , Matthew A. LARSEN , Kun LIU , Ping LIU , Umar Faruk MANSOOR , Jianping PAN , Christopher W. PLUMMER , Aaron SATHER , Uma SWAMINATHAN , Huijun WANG , Merck Sharp & Dohme Corp.
发明人： Yonglian Zhang , Amjad Ali , Jared Cumming , Duane DeMong , Qiaolin Deng , Thomas H. Graham , Elisabeth Hennessy , Matthew A. Larsen , Kun Liu , Ping Liu , Umar Faruk Mansoor , Jianping Pan , Christopher W. Plummer , Aaron Sather , Uma Swaminathan , Huijun Wang
IPC分类号： A61K31/519 , A61K39/395 , C07D471/04 , C07D519/00 , A61K31/55
摘要： In its many embodiments, the present invention provides certain 7-, 8-, and 10-substituted amino triazolo quinazoline derivatives of Formula (I): or a pharmaceutically acceptable salt thereof, wherein ring A, R1, R2, and R4 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutic agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and their use in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.
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公开(公告)号：US08735435B2
公开(公告)日：2014-05-27
申请号：US12625783
申请日：2009-11-25
申请人： Amjad Ali , Joann M. Napolitano , Qiaolin Deng , Zhijian Lu , Peter J. Sinclair , Gayle E. Hallett , Christopher F. Thompson , Nazia Quraishi , Cameron J. Smith
发明人： Amjad Ali , Joann M. Napolitano , Qiaolin Deng , Zhijian Lu , Peter J. Sinclair , Gayle E. Hallett , Christopher F. Thompson , Nazia Quraishi , Cameron J. Smith
IPC分类号： C07D263/04 , A61K31/421
CPC分类号： C07F7/10 , A61K31/4015 , A61K31/4166 , A61K31/4168 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K45/06 , C07D207/26 , C07D207/27 , C07D233/32 , C07D233/38 , C07D233/50 , C07D233/52 , C07D263/04 , C07D263/20 , C07D263/22 , C07D263/24 , C07D263/26 , C07D285/06 , C07D285/10 , C07D401/04 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/04 , C07D417/10
摘要： Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.
摘要翻译： 具有式I结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于升高HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。在式I化合物中，B或 R2是具有邻芳基，杂环，苯并杂环或苯并环烷基取代基的苯基，并且在5元环上的另一个位置具有直接连接到环上或连接到环上的芳族，杂环，环烷基，苯并杂环或苯并环烷基取代基 通过-CH2-。
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公开(公告)号：US07652049B2
公开(公告)日：2010-01-26
申请号：US11173295
申请日：2005-07-01
申请人： Amjad Ali , Joann M. Napolitano , Qiaolin Deng , Zhijian Lu , Peter J. Sinclair , Gayle E. Taylor , Christopher F. Thompson , Nazia Quraishi , Cameron J. Smith , Julianne A. Hunt , Adrian A. Dowst , Yi-Heng Chen , Hong Li
发明人： Amjad Ali , Joann M. Napolitano , Qiaolin Deng , Zhijian Lu , Peter J. Sinclair , Gayle E. Taylor , Christopher F. Thompson , Nazia Quraishi , Cameron J. Smith , Julianne A. Hunt , Adrian A. Dowst , Yi-Heng Chen , Hong Li
IPC分类号： C07D263/20 , A61K31/4015
CPC分类号： C07F7/10 , A61K31/4015 , A61K31/4166 , A61K31/4168 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K45/06 , C07D207/26 , C07D207/27 , C07D233/32 , C07D233/38 , C07D233/50 , C07D233/52 , C07D263/04 , C07D263/20 , C07D263/22 , C07D263/24 , C07D263/26 , C07D285/06 , C07D285/10 , C07D401/04 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/04 , C07D417/10
摘要： Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.
摘要翻译： 具有式I结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于升高HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。在式I化合物中，B或 R2是具有邻芳基，杂环，苯并杂环或苯并环烷基取代基的苯基，并且在5元环上的另一个位置具有直接连接到环上或连接到环上的芳族，杂环，环烷基，苯并杂环或苯并环烷基取代基 通过-CH2-。
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公开(公告)号：US20080119476A1
公开(公告)日：2008-05-22
申请号：US11631821
申请日：2005-07-01
申请人： Amjad Ali , Joann M. Napolitano , Qiaolin Deng , Zhijian Lu , Peter J. Sinclair , Gayle E. Taylor , Christopher F. Thompson , Nazia Quraishi , Cameron J. Smith , Julianne A. Hunt , Adrian A. Dowst , Yi-Heng Chen , Hong Li
发明人： Amjad Ali , Joann M. Napolitano , Qiaolin Deng , Zhijian Lu , Peter J. Sinclair , Gayle E. Taylor , Christopher F. Thompson , Nazia Quraishi , Cameron J. Smith , Julianne A. Hunt , Adrian A. Dowst , Yi-Heng Chen , Hong Li
IPC分类号： A61K31/422 , A61K31/40 , A61K31/4166 , A61K31/427 , A61K31/4439 , A61K31/501 , A61P9/10 , C07D233/32 , C07D263/20 , C07D417/10 , C07D417/04 , C07D413/10 , C07D413/04 , C07D401/04 , C07D285/10 , C07D233/44 , C07D207/24 , A61K31/506 , A61K31/497 , A61K31/433 , A61K31/4168 , A61K31/421
CPC分类号： C07F7/10 , A61K31/4015 , A61K31/4166 , A61K31/4168 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K45/06 , C07D207/26 , C07D207/27 , C07D233/32 , C07D233/38 , C07D233/50 , C07D233/52 , C07D263/04 , C07D263/20 , C07D263/22 , C07D263/24 , C07D263/26 , C07D285/06 , C07D285/10 , C07D401/04 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/04 , C07D417/10
摘要： Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.
摘要翻译： 具有式I结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于升高HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。在式I化合物中，B或 R 2是具有邻芳基，杂环，苯并杂环或苯并环烷基取代基的苯基，并且在5元环上的另一个位置具有直接连接的芳族，杂环，环烷基，苯并杂环或苯并环烷基取代基 通过-CH 2 - 2连接到环上或连接到环上。
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公开(公告)号：US20070225365A1
公开(公告)日：2007-09-27
申请号：US11578694
申请日：2005-04-08
申请人： Amjad Ali , Joann Bohn , Qiaolin Deng , Zhijian Lu , Peter Sinclair , Gayle Taylor , Christopher Thompson , Nazia Quraishi
发明人： Amjad Ali , Joann Bohn , Qiaolin Deng , Zhijian Lu , Peter Sinclair , Gayle Taylor , Christopher Thompson , Nazia Quraishi
IPC分类号： A61K31/216 , C07C69/612
CPC分类号： C07C271/20 , C07C233/18 , C07C271/16 , C07C271/22 , C07C279/08 , C07C311/04 , C07C311/08 , C07C317/32 , C07D209/08 , C07D213/40 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/89 , C07D215/12 , C07D215/26 , C07D217/02 , C07D217/14 , C07D261/08 , C07D271/06 , C07D307/52 , C07D307/79 , C07D333/20 , C07D333/22 , C07D333/28
摘要： Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula 1, A1 and A2 are each an aromatic ring, a 5-6-membered heterocyclic ring, an aromatic ring fused to a heterocyclic ring, a phenyl ring fused to a heterocyclic ring, or a cycloalkyl ring.
摘要翻译： 式I化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于培养HDL-胆固醇，降低LDL-胆固醇，以及治疗或预防动脉粥样硬化。 在式1化合物中，A 1和A 2各自为芳环，5-6元杂环，稠合至杂环的芳环， 与杂环稠合的苯环或环烷基环。
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